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Chlorphenamine
| InChI = 1/C16H19ClN2/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13/h3-9,11,15H,10,12H2,1-2H3 | smiles = Clc1ccc(cc1)C(c2ncccc2)CCN©C | InChIKey = SOYKEARSMXGVTM-UHFFFAOYAD | CAS_number = 132-22-9 | ChemSpiderID = 2624 | ATC_prefix = R06 | ATC_suffix = AB04 | PubChem = 2725 | DrugBank = DB01114 | C = 16 |H = 19 |Cl = 1 |N = 2 | molecular_weight = 274.788 g/mol | bioavailability = 25 to 50% | solubility = 0.55 g/100 mL, liquid | protein_bound = 72% | metabolism = Hepatic (CYP2D6) | elimination_half-life = 21-27 hours | excretion = Renal | pregnancy_AU = A | pregnancy_US = B | pregnancy_category = | legal_AU = S3 | legal_UK = GSL | legal_US = OTC | legal_status = (für oral forms, 口服劑) | routes_of_administration = Oral, IV, IM, SC / 口服、靜脈注射、肌肉注射、皮下注射 }} Chlorpheniramine is part of a series of antihistamines including pheniramine (Naphcon) and its halogenated derivatives and others including fluorpheniramine, dexchlorpheniramine (Polaramine), brompheniramine (Dimetapp), dexbrompheniramine (Drixoral), deschlorpheniramine, dipheniramine (also known as triprolidine with the trade name Actifed), and iodopheniramine. The halogenated alkylamine antihistamines all exhibit optical isomerism, and chlorpheniramine in the indicated products is racemic chlorpheniramine maleate, whereas dexchlorpheniramine (Polaramine) is the dextrorotary stereoisomer. It is also known as Comakin in Taiwan and parts of Asia. 適應症及用量 減輕過敏症狀，例如過敏性鼻炎（包括花粉症）、荨麻疹等。氯苯那敏可減輕流鼻涕及噴嚏。用於口服時，成人劑量通常是每4至6小時服4毫克。 不良反應 主要是容易令人產生睡意，其它比較常見的不良反應有頭痛、小便滯留、口乾、腸胃不適等。 Serotonergic and norepinephrinergic effects In addition to being an H-1 histamine receptor antagonist, chlorpheniramine has been shown to work as a serotonin-norepinephrine reuptake inhibitor or SNRI. Carlsson A., Linqvist M. (1969). Central and peripheral monoaminergic membrane-pump blockade by some addictive analgesics and antihistamines. J Pharm Pharmacol 1969; 21: 460–4. A similar antihistamine, brompheniramine, led to the discovery of the SSRI zimelidine. Limited clinical evidence shows that it is comparable to several antidepressant medications in its ability to inhibit the reuptake of serotonin and also norepinephrine (noradrenaline). Hellbom, E. (2006). Chlorpheniramine, selective serotonin-reuptake inhibitors (SSRIs) and over-the-counter (OTC) treatment. Medical Hypotheses, 2006; 66(4), 689 - 690. However, extensive clinical trials of its psychiatric properties in humans have not been conducted. It inhibits serotonin reuptake less than norepinephrine reuptake, Edward F. Domino (1999). History of Modern Psychopharmacology: A Personal View With an Emphasis on Antidepressants. Psychosomatic Medicine 1999; 61:591-598. however the literature is not consistent in this respect (compare Hellbom (2005) with Domino (1999)). Combination medications Chlorpheniramine is often combined with phenylpropanolamine to form an allergy medication with both antihistamine and decongestant properties. Brand names include Demazin, Allerest 12 Hour, Codral Nighttime, Chlornade, Contac 12 Hour, A. R. M. Allergy Relief, Ordrine, Ornade Spansules, Teldrin, Triaminic, and Tylenol Cold/Allergy. Chlorpheniramine is combined with a narcotic (hydrocodone) in the product Tussionex, which is indicated for treatment of cough and upper respiratory symptoms associated with allergy or cold in adults and children 6 years of age and older.UCB : Tussionex (Respiratory Disease). 2007. UCB, Inc.. 11 Jul 2008 . This combination is manufactured as a time-released formula, which allows for administration every 12 hours, versus the more common 4-to-6-hour regimen for other narcotic cough suppressants. Chlorpheniramine/Dihydrocodeine immediate-release syrups are also marketed. The antihistamine is helpful in cases where allergy or common cold is the reason for the cough; it is also a potentiator of opioids, allowing enhanced suppression of cough, analgesia, and other effects from a given quantity of the drug by itself. In various places in the world, cough & cold preparations containing codeine and chlorpheniramine are available. In the drug Coricidin, Chlorphenamine is combined with the cough suppressant dextromethorphan. References / Riförènses / 參考資料 See also / Si osou / 參看 * Diphenhydramine * Dexchlorpheniramine External link / Ikstörnol liŋk / 外部連結 * Category:World Health Organization essential medicines Category:Pyridines Category:Organochlorides Category:H1 receptor antagonists Category:Serotonin-norepinephrine reuptake inhibitors Chlorphenamine